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entecavir (Rx)Brand and Other Names:Baraclude

 
 
 

Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 0.5mg
  • 1mg

oral solution

  • 0.05mg/mL
more...

Chronic Hepatitis B

Indicated for treatment of CHB with evidence of active viral replication and either evidence of persistent elevations in serum aminotransferases (ALT or AST) or histologically active disease

Nucleoside inhibitor treatment-naïve with compensated liver disease (adults and adolescents ≥16 yr): 0.5 mg PO qDay

Lamivudine-refractory or known lamivudine or telbivudine resistance substitutions (adults and adolescents ≥16 yr): 1 mg PO qDay

Decompensated liver disease (adults): 1 mg PO qDay

Indication is based on the following

  • Histologic, virologic, biochemical, and serologic responses in nucleoside-treatment-naïve and lamivudine-resistance with HBeAg-positive or HBeAg-negative chronic HBV infection and compensated liver disease
  • Virologic, biochemical, serologic, and safety data are available from a controlled study with chronic HBV infection and decompensated liver disease
  • Virologic, biochemical, serologic, and safety data are available for a limited number of adults with HIV/HBV coinfection who have received prior lamivudine therapy

Renal Impairment

Usual daily dose (0.5 mg)

  • CrCl ≥50 mL/min: No dosage adjustment required
  • CrCl 30-49 mL/min: Reduce to 0.25 mg/day or 0.5 mg q48hr
  • CrCl 10-29 mL/min: Reduce to 0.15 mg/day or 0.5 mg q72hr
  • CrCl <10 mL/min, hemodialysis, or CAPD: 0.05 mg/day or 0.5 mg q7days

Lamivudine-refractory/decompensated liver disease daily dose (1 mg)

  • CrCl ≥50 mL/min: No dosage adjustment required
  • CrCl 30-49 mL/min: Reduce to 0.5 mg/day or 1 mg q48hr
  • CrCl 10-29 mL/min: Reduce to 0.3 mg/day or 1 mg q72hr
  • CrCl <10 mL/min, hemodialysis, or CAPD: 0.1 mg/day or 1 mg q7days

Administration

Take on empty stomach (2 hr AC or PC)

Use oral solution when needed for renal impairment dosage adjustments

Dosage Forms & Strengths

tablet

  • 0.5mg
  • 1mg

oral solution

  • 0.05mg/mL
more...

Chronic Hepatitis B

Indicated for treatment of CHB with evidence of active viral replication and either evidence of persistent elevations in serum aminotransferases (ALT or AST) or histologically active disease in children ≥2 years and weigh at least 10 kg

<2 years: Safety and efficacy not established

≥16 years: As adult

Nucleoside inhibitor treatment-naïve

  • Administer PO once daily
  • 10-11 kg: 0.15 mg (3 mL)
  • >11-14 kg: 0.2 mg (4 mL)
  • >14-17 kg: 0.25 mg (5 mL)
  • >17-20 kg: 0.3 mg (6 mL)
  • >20-23 kg: 0.35 mg (7 mL)
  • >23-26 kg: 0.4 mg (8 mL)
  • >26-30 kg: 0.45 mg (9 mL)
  • >30 kg: 0.5 mg (10 mL oral solution or one 0.5-mg tab)

Lamivudine-experienced

  • Administer PO once daily
  • 10-11 kg: 0.3 mg (6 mL)
  • >11-14 kg: 0.4 mg (8 mL)
  • >14-17 kg: 0.5 mg (10 mL)
  • >17-20 kg: 0.6 mg (12 mL)
  • >20-23 kg: 0.7 mg (14 mL)
  • >23-26 kg: 0.8 mg (16 mL)
  • >26-30 kg: 0.9 mg (18 mL)
  • >30 kg: 1 mg (20 mL oral solution or one 1-mg tab)

Renal Impairment

Insufficient data exist to recommend a specific dose adjustment in pediatric patients with renal impairment

Consider dose reductions or dosing interval increases similar to adult adjustments

Administration

Take on empty stomach (2 hr AC or PC)

Use oral solution for children weighing 10-30 kg

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Adverse Effects

1-10%

Fatigue (1-3%)

Headache (2-4%)

Dizziness

Nausea

<1%

Diarrhea

Dyspepsia

Vomiting

Somnolence

Insomnia

Postmarketing Reports

Lactic acidosis

Increased transaminases

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Warnings

Black Box Warnings

Severe acute exacerbations of hepatitis reported following discontinuing drug; monitor hepatic function

Resistance to HIV NRTIs may emerge in patients with chronic hepatitis B in whom HIV infection is unrecognized or untreated

Not for HIV/HBV coinfected patients unless being treated with highly active antiretroviral therapy (HAART)

Lactic acidosis and severe hepatomegaly with steatosis, including fatal cases, reported

Do not use Epivir HBV tablets or solution to treat HIV

Contraindications

Hypersensitivity

Cautions

Discontinuation may result in acute exacerbation of hepatitis B

Caution in liver transplant recipients or renal impairment

Pregnancy

Risk of HIV resistance: not recommended for HIV/HBV coinfected patients who are not also receiving HAART

Patients with decompensated liver disease may be at greater risk for lactic acidosis

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Pregnancy & Lactation

Pregnancy Category: C

Lactation: excretion in milk unknown/not recommended

Pregnancy Registry: Healthcare providers are encouraged to register pregnant women exposed to entecavir by calling 1-800-258-4263.

Pregnancy Categories

A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA:Information not available.

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Pharmacology

Mechanism of Action

Selective HBV DNA polymerase inhibitor; inhibition blocks reverse transcriptase activity, which in turn reduces viral DNA synthesis

Pharmacokinetics

Half-Life, Elimination: 5-6 days

Peak Plasma Time: 0.5-1.5 hr

Peak Plasma Concentration: 0.5 mg dose: 4.2 ng/mL; 1 mg dose: 8.2 ng/mL

Distribution: Extensively in tissues

Protein Bound: 13%

Metabolism: Not a substrate, inducer or inhibitor of the Cytochrome P450 system

Excretion: Primarily urine

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Images

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Formulary

FormularyPatient Discounts

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The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

Tier Description
1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
NC NOT COVERED – Drugs that are not covered by the plan.
Code Definition
PA Prior Authorization
Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
QL Quantity Limits
Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
ST Step Therapy
Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
OR Other Restrictions
Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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